The overall objective of this proposal is to preclinically develop VMD-1201 or a lead analog compound of a preferentially peripheral-acting PKC epsilon inhibitor as an oral targeted anticancer drug for treatment of human head and neck cancer with much reduced side effects. The long term goal of this developmental project is to develop this mechanism-based PKC epsilon specific inhibitor, through preclinical and human clinical trials, as an effective oral drug for advanced human head and neck cancer.